Hypochlorous acid-based eyelid cleansers

ABSTRACT

An antimicrobial eyelid cleanser composition contains: (a) a hypohalous acid; (b) one or more surfactants having a HLB value of 5 to 18; and (c) an aqueous vehicle, the aqueous vehicle comprising: (i) one or more tonicity adjusters; (ii) one or more osmolality adjusters for adjusting an osmolality of the composition; and (iii) one or more pH adjusters for maintaining the pH of the composition at between about 4.5 to about 8.0. The composition can be dispensed in a foam, liquid, spray, mist, gel or lotion form. The composition can facilitate long term eyelid hygiene by removing excess oil, debris and desquamated skin and provide relief for inflammation of the eyes.

CROSS-REFERENCE TO RELATED APPLICATIONS

This application claims the benefit of Provisional U.S. PatentApplication No. 62/665,930 filed May 2, 2018, and entitled “HypochlorousAcid-Based Eyelid Cleansers,” the entire content and disclosure ofwhich, both express and implied, is incorporated herein by reference.

FIELD OF THE INVENTION

The present invention relates generally to eyelid and skin cleaningcompositions and to methods of preparing and using such compositions.

BACKGROUND

Ocular health refers to eyes as well as structures associated with theeyes, eyelids for example. The eyelids are important in over-all ocularhealth because they protect the eyes from dangers such as approachingobjects or from airborne contaminants, such as pollen, dust particles orother foreign bodies. The eyelids contain essential glands; the lacrimalglands and meibomian glands that produce layers of tear film that arecritical for healthy eyes. When an individual blinks, a new tear film iscreated and tears are distributed across the cornea to lubricate thesurface of the eye. This blinking action also “flushes” foreignmaterials from the eye.

The eyelids, however, are subject to certain problems, which while verycommon, are none-the-less bothersome, especially for contact lenswearers, and may lead to other more serious complications. Onecomplication is blepharitis. Blepharitis is a common chronicinflammation of the eyelids characterized by a scaly crust on the lidmargins. The condition may be caused by a bacterial infection, or it maybe allergic in origin or associated with seborrhea of the face andscalp. Treatment usually involves cleansing the eyelids on a regularbasis to remove excess oil, debris, and desquamated skin that may beproblematic.

Often associated with or secondary to blepharitis is a bacterialinfection of the surface of the skin at the edge of the lid known as aninternal hordeolum. Other such infections include external hordeolum,commonly referred to as styes, which are infections of the tiny oilsecreting meibomian glands along the edge of the eyelid, surrounding theeyelashes. A stye begins as a red, tender bump and usually fullydevelops within three days. Such conditions are accompanied by pain,redness and tenderness of the eyelid (or lid) margins. Although styesare often recurring, regular cleansing of the eyelid margins canminimize such conditions. A second problem is a chalazion, which is aninflammation of the meibomian glands inside the eyelid. Chalaziatypically grow slowly over 2-3 weeks and although they do not typicallycause pain, they often require surgical intervention if left untreated.

With any of the above-described problems, as well as other medicalcomplications, such as rosacea and seborrhea, proper eyelid hygiene withthe use of an eyelid cleanser may minimize the severity of the outbreak,or prevent the problem altogether if caught early. Eyelid cleansers arealso used for cleaning eyelashes, eyelids or the periocular area and maybe used as a pre-operative scrub to help reduce the presence of harmfulbacteria which may cause infection, inflammation, or evenendophthalmitis in patients.

SUMMARY

Compositions containing hypochlorous acid and water have been usedsuccessfully along with other eyelid care compositions to facilitatelong term eyelid hygiene, as has been described in Applicant's U.S. Pat.No. 9,833,399. However, Applicant has determined that there is a needfor a single isotonic/isoosmolar and physiologically compatibleanti-microbial formulation that can also provide the cleansing effectsof a surfactant-based formulation.

In an embodiment, an eyelid cleanser composition contains: (a) ahypohalous acid; (b) one or more surfactants having a HLB value of 5 to18; and (c) an aqueous vehicle, the aqueous vehicle comprising: (i) oneor more tonicity adjusters; (ii) one or more osmolality adjustersconfigured to adjust an osmolality of the composition; and (iii) one ormore pH adjusters for adjusting the pH of the composition at betweenabout 4.5 to about 8.0. The composition can be dispensed in a foam,liquid, spray, mist, gel or lotion form. The composition can facilitatelong term eyelid hygiene by removing excess oil, debris and desquamatedskin and also provide relief for inflammation of the eyes.

In a preferred embodiment, the hypohalous acid is hypochlorous acid. Thecomposition can contain from 10 to 1000 ppm of hypochlorous acid. Incertain embodiments, the composition contains from 50 to 300 ppm ofhypochlorous acid.

Preferably, the composition has one or more surfactants having a HLBvalue from 10-18. When the composition includes a combination ofsurfactants, at least a first surfactant has a HLB value from 10 to 18and a second surfactant has a HLB value from 5-10. The one or moresurfactants are selected from the group consisting of nonionic andamphoteric surfactants. In certain embodiments, the one or moresurfactants are selected from the group consisting of sorbitan, sorbitanmonolaurate, polyoxyethylene or polyethylene glycol (PEG) modifiedmolecules such as PEG-modified surfactants, PEG-modified phospholipids,PEG-modified sugars, amineoxides, block copolymers and mixtures thereof.A total concentration of the one or more surfactants in the compositionis in the range of 0.01 to 20% w/w of the total composition. In certainembodiments, the total concentration of the one or more surfactants inthe composition is in the range of 0.01-5% w/w.

The composition is physiologically compatible and isotonic/isoosmolar.The tonicity adjuster can be selected from the group consisting ofsodium chloride, potassium chloride, calcium chloride, magnesiumchloride, sodium lactate, potassium lactate, calcium lactate andmixtures thereof.

The osmolality adjusters are configured to adjust an osmolality of thecomposition from 100 mOsm/kg to 500 mOsm/kg. The osmolality adjusterscan be selected from the group consisting of sugars, glycerin, propyleneglycol and mixtures thereof.

In one or more embodiments, the composition contains a foam stabilizer.The foam stabilizer can be a polyethylene glycol diester of methylglucose and a fatty acid.

In one or more embodiments, the composition includes 0.01-5% w/w of oneor more ingredients selected from the group consisting of propyleneglycol, glycerin, liquid polyols, nut oils and derivatives, floralextracts, fruit extracts, sodium alginate, hyaluronic acid,diglycerides, triglycerides, PEG-75 Lanolin, mineral oil, silicone oiland mixtures thereof.

In one or more embodiments, the composition includes 0.01-5% w/w of oneor more ingredients selected from the group consisting of anantioxidant, an anti-irritant, a cooling agent, a viscosity modifier andmixtures thereof.

In another embodiment, a kit for maintaining eyelid hygiene consistsessentially of an applicator and the eyelid cleanser compositiondisclosed herein. The applicator can include a hypoallergenic,non-woven, hydrophilic material.

In yet another embodiment, a kit for maintaining eyelid hygiene consistsessentially of an applicator pre-moistened with an effective amount ofthe eyelid cleanser composition disclosed herein. The applicator caninclude one or more fabric pads, wherein each pad is individuallypackaged in a sealable package.

In another embodiment, a method for managing eyelid care involves theapplication of an effective amount of the eyelid cleanser compositiondisclosed herein to the eyelids and its surrounding areas. Thecomposition can be either left on or rinsed off after application.

DETAILED DESCRIPTION

The term and phrases “invention,” “present invention,” “instantinvention,” and similar terms and phrases as used herein arenon-limiting and are not intended to limit the present subject matter toany single embodiment, but rather encompass all possible embodiments asdescribed.

As used herein, all weight percentages (wt. %) are based on the totalwt. % of the skin care composition, unless otherwise specified.Additionally, all composition percentages are based on totals equal to100 wt. %, unless otherwise specified.

The compositions and methods for their use can “comprise,” “consistessentially of,” or “consist of” any of the ingredients or stepsdisclosed throughout the specification. As used in this specificationand claim(s), the words “comprising” (and any form of comprising, suchas “comprise” and “comprises”), “having” (and any form of having, suchas “have” and “has”), “including” (and any form of including, such as“includes” and “include”) or “containing” (and any form of containing,such as “contains” and “contain”) are inclusive or open-ended and caninclude the ingredients of the present invention and do not excludeother ingredients or elements described herein. The use of the word “a”or “an” when used in conjunction with the term “comprising” in theclaims and/or the specification may mean “one,” but it is alsoconsistent with the meaning of “one or more,” “at least one,” and “oneor more than one.” As used herein, “consisting essentially of” meansthat the invention may include ingredients in addition to those recitedin the claim, but only if the additional ingredients do not materiallyalter the basic and novel characteristics of the claimed invention.Generally, such additives may not be present at all or only in traceamounts. However, it may be possible to include up to about 10% byweight of materials that could materially alter the basic and novelcharacteristics of the invention as long as the utility of thecomposition (as opposed to the degree of utility) is maintained.

All ranges recited herein include the endpoints, including those thatrecite a range “between” two values. Terms such as “about,” “generally,”“substantially,” and the like are to be construed as modifying a term orvalue such that it is not an absolute. Such terms will be defined by thecircumstances and the terms that they modify as those terms areunderstood by those of skill in the art. In one non-limiting embodiment,the terms are defined to be within 5%. The term “substantially” and itsvariations are defined as being largely but not necessarily wholly whatis specified as understood by one of ordinary skill in the art, and inone non-limiting embodiment substantially refers to ranges within0.01%-5%.

As used herein, the term “effective amount” of a composition refers toan amount sufficient to elicit the desired biological response. As willbe appreciated by those of ordinary skill in this art, and effectiveamount of a substance may vary depending on such factors as the desiredbiological endpoint, the patient, etc. The terms effective amount andclinically effect may be used interchangeably herein. For example, aeffective amount/clinically effective amount of the composition is theamount that can be used facilitate long term eyelid hygiene while alsosubstantially reducing inflammation and promoting wound healing of theeyelids.

While the specification concludes with the claims particularly pointingand distinctly claiming the invention, it is believed that the presentinvention will be better understood from the following description.

The eyelid cleanser composition is an ophthalmic/ocular composition thatcan clean the eyelids and eyes and remove excessive oil, debris, anddesquamated skin from the eyelids and surrounding areas while reducinginflammation and promoting wound healing. The composition contains ahypohalous acid, one or more surfactants having a hydrophile-lipophilebalance (HLB) value ranging between 10 and 18, and an aqueous vehiclecontaining one or more components for adjusting the pH, tonicity,osmolality of the composition.

The “hal” of the hypohalous acid is a halogen selected from the groupconsisting of chloro, bromo, iodo and fluoro. Preferably, the halogen ischloro and the hypohalous acid is hypochlorous acid. The compositioncontains at least 10-1000 ppm of hypochlorous acid. In certainembodiments, the composition contains 50-300 ppm of hypochlorous acid.

One or more nonionic or amphoteric surfactants can be used in theformulation to achieve a desired foaming capacity and/or cleansingcapability. The inclusion of a surfactant will enhance the ability ofthe composition to dissolve and remove oil, debris and desquamated skin.Preferable surfactants have a foaming ability and include nonionic oramphoteric surfactants having a HLB value between 10 and 18. If morethan one surfactant is used, then at least one surfactant should has anHLB value between 10 and 18 and the other surfactant(s) should eitherhave an HLB between 10 and 18 or an HLB value between 5 and 10. Suitablesurfactants that may be used include, but are not limited to, sorbitanesters (such as, without limitation, Span 20 or sorbitan monolaurate, orthe polyoxyethylene derivatives of sorbitan esters), polyethylene glycol(PEG) modified surfactants (such as, without limitation, polysorbate 80,Brij 52, PEG-75 Lanolin), modified phospholipids, modified sugars (suchas, without limitation, alkyl polyglucosides, fatty acid glucamides),amineoxides, and/or block copolymers such as, Pluronics (Pluronic F120,Poloxamer 188). The total concentration of surfactants can be in therange of 0.01 to 20% w/w of the final formulation but, more preferablyin the 0.01-5% range.

The aqueous vehicle can be deionized water or purified water USP. Thecomposition is physiologically compatible and isotonic/isoosmolar. Theaqueous vehicle includes one or more components for adjusting tonicity,osmolality and pH, as needed. Preferred tonicity adjusters include oneor more salts, such as, chlorides of sodium, potassium, calcium andmagnesium, and sodium/potassium/calcium lactate. Osmolality can beadjusted using sugars, glycerin, propylene glycol and similaringredients. The osmolality of the composition can be adjusted fromabout 100 mOsm/kg to about 500 mOsm/kg. In certain embodiments, theosmolality of the composition is maintained at about 180 to about 400mOsm/kg. The osmolality adjuster can include sugars, glycerin, propyleneglycol and mixtures thereof and other similar ingredients.

Optimally, the pH of the composition is kept between 4.5 and 8.5, orpreferably between a pH range between 5.0 and 7.0. The pH can beadjusted without the use of traditional pH adjusters which can beirritating to the eye. For instance, the pH of the composition may beadjusted by adding buffering components such as phosphate salts, citratesalts, tris salts and the corresponding acids/bases in defined ratios totarget the desired pH when the aqueous vehicle is prepared or by addingincremental amounts of an acid or a base with stirring until the desiredpH is reached once all ingredients have been dissolved/dispersed.

The inclusion of hypochlorous acid provides the composition with anantimicrobial activity. The antimicrobial activity will vary dependingon the concentration of hypochlorous acid, the presence of one or moresurfactants, and the pH of the composition. Maintaining the pH of thecomposition will also optimize the stability of the hypochlorous acid,its antimicrobial activity, and reduce any negative reactions with theskin or eyelid if applied to the eyelid or skin and not washed off.

Although optional, a foam stabilizer can be added to the composition,and may include, without limitation, a polyethylene glycol diester ofmethyl glucose and a fatty acid. The fatty acid can be selected from agroup consisting of oleic acid, stearic acid, lauric acid, caprylicacid, and capric acid. Preferably, the one or more foam stabilizersincludes PEG-120 methyl glucose dioleate.

The composition can also include additional components in amounts up toa 5% w/w of the composition. These components include one or moremoisturizers, emollients, humectants, or lubricants are also commonlyadded to the composition and are generally referred to herein asmoisturizers. Suitable moisturizers are propylene glycol, glycerin,polyethylene glycol (e.g. PEG 300, 400, 600) or generally, liquidpolyols, nut oils and derivatives, floral extracts, such as, roseextracts, fruit extracts such as cucumber extract, sodium alginate,hyaluronic acid, medium chain diglycerides, medium chain triglycerides,PEG-75 lanolin, mineral oil, silicone oil and mixtures thereof.

The composition further includes up to 5% w/w of one or more optionalcomponents including such compounds as antioxidants (such as, withoutlimitation, Vitamin E and its derivatives, green tea extract, Vitamin Cand its derivatives), anti-irritating/soothing agents (such as, withoutlimitation, allantoin, aloe vera, tea tree oil), cooling agents (suchas, without limitation, sorbitol, xylitol, menthol, thymol), andviscosity modifiers (such as, without limitation, carboxymethylcellulose, hydroxypropyl methylcellulose, Carbopol®). The viscosity ofthe composition is preferably greater than 10 cps. In certainembodiments, the viscosity can also be in the range of 1-10 cps.

In an embodiment, a method of manufacturing the composition isdisclosed. The method involves mixing the ingredients disclosed hereininto the aqueous vehicle in order of increasing concentration withconstant mixing (low shear) until all water-miscible/water-solubleingredients are homogenously dissolved/dispersed within the vehicle. Inthe embodiments that involve oil soluble ingredients, a separate oilphase may be prepared (at 30-70° C.) and then added to the aqueous phasewith vigorous stirring at 30-70° C. (depending on stability ofingredients) until a homogenous dispersion is formed.

The eyelid cleanser composition is typically applied to the surface ofthe eyelid and surrounding areas in the form of a spray, mist, foam orgel. In certain embodiments, the composition may be applied for aduration/frequency prescribed by a physician. The composition may beeither left on the surface of the eyelid or surrounding areas or it canbe wiped off after use. Whenever, the composition is used as a wipe-offformula, a hypoallergenic non-woven, hydrophilic material is recommendedfor best results. The composition can be configured to be non-residueforming. The composition is not to be used on open wounds, scars, orvisible signs of inflammation, eczema and allergic rash. The compositioncan be clear to translucent and be colorless to yellowish in appearance.

The eyelid cleanser composition can be contained and dispensed from asuitable receptacle/dispenser. In certain embodiments, the container isa pump dispenser configured to contain and deliver the eyelid cleansercomposition as a pre-lathered foam. The eyelid cleanser composition canbe selected from a group consisting of a solution, a foam, a gel, aspray, a lotion, a suspension, an emulsion, microemulsion, an ointmentand combinations thereof. In certain embodiments, the composition may bebiphasic, that is, having two distinct separate layers within acontainer that has to be shaken before application.

In certain embodiments, an eyelid cleaning kit can include one or morefabric pads or wipes impregnated/pre-moistened with a clinicallyeffective amount of the eyelid cleanser composition. The term “pad”refers to a thick piece of fabric that is capable of holding orabsorbing the eyelid cleanser composition. For example, the fabric canbe a lint-free fabric, such as, rayon or another suitable material. Incertain embodiments, the fabric pad may be a cotton pad. The pads may besingle use disposable pads. The kit can also include between 1-100 pads.The pads may be sealed individually or wrapped within any suitablepackaging.

In certain embodiments, the kit can include one or more single use drypads. A desired amount of the eyelid cleanser composition may then beapplied to a dry pad prior to using it to cleanse the eyelids. Inanother embodiment, the kit can include a swab or another suitableapplicator/system that can be saturated with a desired amount of theeyelid cleanser composition.

It will be apparent to those skilled in the art that variousmodifications and variations can be made in the present inventionwithout departing from the scope or spirit of the invention. Otherembodiments of the invention will be apparent to those skilled in theart from consideration of the specification and practice of theinvention disclosed herein. It is intended that the specification andexamples be considered as exemplary only.

What is claimed is:
 1. An eyelid cleanser composition comprising: (a) ahypohalous acid; (b) a combination of surfactants, wherein (i) a firstsurfactant has a HLB value from 10 to 18, and (ii) a second surfactanthas a HLB value from 5-10; and (c) an aqueous vehicle, the aqueousvehicle comprising: (i) one or more tonicity adjusters; (ii) one or moreosmolality adjusters for adjusting an osmolality of the composition; and(iii) one or more pH modifiers for adjusting a pH of the composition tobetween about 4.5 to about 8.0, wherein a total concentration of thecombination of surfactants in the composition is in the range of 0.01 to20% w/w.
 2. The eyelid cleanser composition according to claim 1,wherein the hypohalous acid is hypochlorous acid, and wherein thecomposition contains from 10 to 1000 ppm of hypochlorous acid.
 3. Theeyelid cleanser composition according to claim 1, wherein the hypohalousacid is hypochlorous acid, and wherein the composition contains from 50to 300 ppm of hypochlorous acid.
 4. The eyelid cleanser compositionaccording to claim 1, wherein the first and second surfactants areselected from the group consisting of nonionic and amphotericsurfactants.
 5. The eyelid cleanser composition according to claim 4,wherein the first and second surfactants are selected from the groupconsisting of sorbitan, sorbitan monolaurate, polyoxyethylene orpolyethylene glycol (PEG) modified molecules such as PEG-modifiedsurfactants, PEG-modified phospholipids, PEG-modified sugars,amineoxides, block copolymers and mixtures thereof.
 6. The eyelidcleanser composition according to claim 1, wherein a total concentrationof the first and second surfactants in the composition are in the rangeof 0.01-5% w/w.
 7. The eyelid cleanser composition according to claim 1,wherein the tonicity adjuster is selected from the group consisting ofsodium chloride, potassium chloride, calcium chloride, magnesiumchloride, sodium lactate, potassium lactate, calcium lactate andmixtures thereof.
 8. The eyelid cleanser composition according to claim1, wherein the one or more osmolality adjusters are configured to adjustan osmolality of the composition from about 100 mOsm/kg to about 500mOsm/kg.
 9. The eyelid cleanser composition according to claim 1,wherein the one or more osmolality adjusters is selected from the groupconsisting of sugars, glycerin, propylene glycol and mixtures thereof.10. The eyelid cleanser composition according to claim 1, wherein thecomposition is in a foam, liquid, spray, mist, gel or lotion form. 11.The eyelid cleanser composition according to claim 1, further comprisinga foam stabilizer.
 12. The eyelid cleanser composition according toclaim 11, wherein the foam stabilizer is a polyethylene glycol diesterof methyl glucose and a fatty acid.
 13. The eyelid cleanser compositionaccording to claim 1, further comprising 0.01-5% w/w of one or moreingredients selected from the group consisting of propylene glycol,glycerin, liquid polyols, nut oils and derivatives, floral extracts,fruit extracts, sodium alginate, hyaluronic acid, diglycerides,triglycerides, PEG-75 Lanolin, mineral oil, silicone oil and mixturesthereof.
 14. The eyelid cleanser composition according to claim 1,further comprising 0.01-5% w/w of one or more ingredients selected fromthe group consisting of an antioxidant, an anti-irritant, a coolingagent, a viscosity modifier and mixtures thereof.
 15. A kit formaintaining eyelid hygiene, wherein the kit consists essentially of anapplicator and the eyelid cleanser composition according to claim
 1. 16.The kit according to claim 15, wherein the applicator comprises ahypoallergenic, non-woven, hydrophilic material.
 17. A kit formaintaining eyelid hygiene, wherein the kit consists essentially of anapplicator pre-moistened with a clinically effective amount of theeyelid cleanser composition according to claim
 1. 18. The kit formaintaining eyelid hygiene according to claim 17, wherein the applicatorcomprises one or more fabric pads, wherein each pad is individuallypackaged in a sealable package.
 19. A method for managing eyelid care,the method comprising the application of an effective amount of theeyelid cleanser composition according to claim 1 to the eyelids and itssurrounding areas.